AZD0364 Chemical Properties

Boiling point:

716.0±70.0 °C(Predicted)

Density 

1.45±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:41.67(Max Conc. mg/mL);84.27(Max Conc. mM)
DMF:25.0(Max Conc. mg/mL);50.56(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.01(Max Conc. mM)
Ethanol:54.5(Max Conc. mg/mL);110.21(Max Conc. mM)

form 

A crystalline solid

pka

2?+-.0.10(Predicted)

color 

White to off-white

InChIKey

HVIGNZUDBVLTLU-MRXNPFEDSA-N

SMILES

C12=NC(C3C(C)=CN=C(NC4N(C)N=CC=4)N=3)=CN1C[C@H](COC)N(CC1=CC=C(F)C(F)=C1)C2=O

AZD0364 Usage And Synthesis

Uses

Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.

Biological Activity

AZD0364 (ATG-017) is an ERK1/2 inhibitor with IC50 of 0.6 nM for ERK2.

in vitro

AZD0364 has high cellular activity against direct downstream substrates of the MAPK signaling pathway (as in BRAF.

in vivo

AZD0364 has good oral pharmacokinetics in various species. In a xenograft model, AZD0364 inhibited phosphorylated p90RSK1 in a concentration-dependent manner in tumors. AZD0634 induces tumor regression in a KRAS-mutated NSCLC Calu 6 xenograft model, in which AZD0634 can be safely and effectively administered in combination with selumetinib.

target

IC 50

ERK2: 0.6 nM (IC₅₀)

References

[1] WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1.

AZD0364(2097416-76-5)Related Product Information

• AZD-5672
• CCR1 antagonist
• AZD-7648
• AZD5153
• AZD-8055
• AZD-0284
• AZD-5305
• AZD 3759
• 2-Pyridinecarboxamide, 6-fluoro-5-[4-[(5-fluoro-3,4-dihydro-2-methyl-3-oxo-6-quinoxalinyl)methyl]-1-piperazinyl]-N-methyl-
• AZD3839 hemifuMarate
• KGZHRAVDXGQUQM-WCQGTBRESA-N
• (S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine
• AZD-2858
• AZD-0156